SYNTHESIS AND ANTITUBERCULAR ACTIVITY OF SOME MANNICH BASES DERIVED FROM ISATIN ISONICOTINIC ACID HYDRAZONE

Document Type : Original Article

Authors

1 Department of Pharmaceutical Organic Chemistry

2 Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy

3 Department of Animal hygiene and Zoonoses, Faculty of Veterinary Medicine, Assiut University, Assiut-71526, Egypt

Abstract

The purpose of this study based on the design and synthesis of a new series of 4-[1(substitutedaminomethyl)]-2-oxo-2,3-dihydro-1H-3-indolylidene-pyridine- carboxylic acid hydrazones (2a-g) in a trial to overcome the resistance developed with the therapeutic uses of isonicotinic acid hydrazide (isoniazid, INH). The new compounds were prepared by reacting isatin isonicotinic acid hydrazone with formalin and the appropriate secondary amines. The structures of the newly synthesized compounds were elucidated using different spectral data (IR, 1HNMR, and 13CNMR) as well as elemental methods of analyses. The lipophilicity of the synthesized compounds supercedes that of INH as expressed by Clog P. The new compounds (2a-g) as well as INH as a reference drug were tested for their antitubercular activity against bovine Mycobacterium tuberculosis at a dose level of 10 μmol. The tested compounds exhibited comparable inhibitory activity against the tested TB strain comparing to INH a reference drug.

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